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Phenylene derivatives and anti-allergic use thereof

  • US 4,994,479 A
  • Filed: 08/15/1986
  • Issued: 02/19/1991
  • Est. Priority Date: 04/03/1985
  • Status: Expired due to Fees
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Assignment
First Claim
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1. A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof:

  • ##STR175## wherein symbols represent;

    A;

    hydrogen atom, a phenyl group or a phenoxy group;

    n;

    an integer of 3 to 10;

    R1 ;

    hydrogen atom or a lower alkoxy group;

    X1 ;

    a group shown by --CH2 CH2 --, --CH═

    CH--, --CH2 --Y1 -- (wherein Y1 ;

    --O--, --S-- or --NH--), --Y1 --CH2, --CO--Y2 -- (wherein Y2 ;

    --NH--, --CH2 --Y1 -- or --Y1 --CH2 --) or --Y2 --CO--;

    a group represented by;

    ##STR176## wherein;

    R2 ;

    a hydrogen atom, a halogen atom, a nitro group, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a lower alkyl group, a hydroxy-lower alkyl group, a lower alkoxycarbonyl-lower alkyl group, a carboxy-lower alkylthio-lower alkyl group, a lower alkoxycarbonyl-lower alkylthio-lower alkyl group, a halo-lower alkyl group, a carboxyl-lower alkoxy group, a lower alkoxycarbonyl-lower alkoxy group, a lower alkanoyl-lower alkoxy group, a lower alkoxycarbonyl-lower alkoxycarbonyl-lower alkoxy group, a lower alkanoyl group or a group represented by the formula;

    ##STR177## (wherein R4 and R5, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a carboxy-lower alkyl group, a lower alkoxycarbonyl-lower alkyl group, a lower alkanoyl group, a carboxy-lower alkanoyl group, a lower alkoxycarbonyl-lower alkanoyl group, a phenyl-lower alkoxy-carbonyllower alkanoyl group, a carbamoyl group, a lower alkoxy oxalyl group or a mono- or di-lower alkylaminocarbonyl group),R3 ;

    a hydrogen atom, a hydroxy group or a lower alkoxy group,X2 ;

    a group represented by --CH═

    CH-- or --Y3 --Y4 -- (wherein Y3 ;

    a single bond, --O--, --S-- or --NH--;

    Y4 ;

    an alkylene group having 1 to 6 carbon atoms which may be intervened by a sulfur atom), andD;

    a carboxy group, or a group represented by;

    ##STR178## with the proviso that;

    (a) when A is hydrogen, B is ##STR179## or ##STR180## (b) when D is carboxy, R2 is a hydrogen atom, a halogen atom, a nitro group, a hydroxy group, a lower alkoxy group, a lower alkyl group, a hydroxy-lower alkyl group, a lower-alkoxy-lower alkyl group, or a halo-lower alkyl;

    X1 ;

    is --CONH--; and

    X2 ;

    is --CH═

    CH-- or --Y3 --Y4 --, wherein Y3 is a single bond or --O--, and Y4 is an alkylene group having 1 to 6 carbon atoms.

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